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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 334 (1986), S. 496-500 
    ISSN: 1432-1912
    Keywords: k-Strophanthines ; Ouabain ; Absorption ; Metabolism ; Elimination ; Man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In 33 healthy male volunteers, given a single oral and intravenous dose of cymarin (k-strophanthin-α), k-strophanthoside (k-strophanthin-γ) and ouabain (g-strophanthin), enteral absorption and renal excretion of these glycosides and their metabolites were investigated by radioimmunoassay and HPLC. Cymarin was absorbed at 47% of the given dose. After intravenous injection 46% and after oral administration 21% of the given dose, i.e. the total amount as detected by radioimmunoassay which consisted of the unchanged glycoside and its metabolites, were excreted by the kidneys mainly as conjugated metabolites. The half-life of elimination, calculated from the total excreted amount was 13 h (i.v.) and 23 h (p.o.), respectively. k-Strophanthoside was absorbed at 16% of the given dose. After i.v.-injection 73% of the given dose was excreted by the kidneys with a half-life of elimination of 99 h. From this total amount about 70% was excreted as the unchanged drug, the remaining 30% as various metabolites. After oral administration 11% of the given dose were excreted with a half-life of elimination of 22 h. 80% of this amount consisted mainly of conjugated k-strophanthoside and conjugated metabolites as k-strophanthin-β, cymarin, k-strophanthidin, cymarol and k-strophanthidol. Only 6% was excreted as the unchanged drug. Ouabain was absorbed after oral administration to a minimum of 1.4%. Given intravenously a total renal excretion of 33% of the given dose with a half-life of elimination of 23 h was measured. Of this 80% was unchanged ouabain. The remaining 20% seemed to be conjugated metabolites which could not be exactly identified.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Documenta ophthalmologica 80 (1992), S. 371-375 
    ISSN: 1573-2622
    Keywords: Cataractoperation ; carteolol ; intraocular pressure ; liposomes (FAT-MLV)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Liposomes are used as carriers providing a prolonged and improved drug action. They are capable of trapping β-blockers such as Carteolol. In a randomized prospective double-blind clinical trial, Carteolol 2% suspended with frozen and thawed multivesicular large vesicles (FAT-MLV), FAT-MLV, and Carteolol 2% were applied to normal (slightly cataracteous) eyes and immediately after extracapsular cataract extraction or phakoemulsiflcation with implantation of a posterior chamber lens in a standard procedure. Twenty-five patients were included in each group. Intraocular pressure (IOP) was measured for 3 days using applanation tonometry. In the normal eyes, a significant reduction of IOP was found for the patients receiving Carteolol and Carteolol MLV suspension. Moreover, an improved action and a prolongation of drug action was registered in the Carteolol/MLV group as compared to Carteolol treatment alone. After cataract operation, the control groups showed a significant increase in IOP. Carteolol produced a constant level of IOP but the Carteolol/MLV suspension showed a stronger decrease after ECCE and a still stronger decrease after phakoemulsification. Hence, Carteolol is suitable for the reduction of IOP but a Carteolol/MLV suspension is more effective, providing the possibility of a single application of a low-dose β-blocker after cataract extraction with posterior chamber lens implantation.
    Type of Medium: Electronic Resource
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